(19)
(11) EP 0 242 052 A3

(12) EUROPEAN PATENT APPLICATION

(88) Date of publication A3:
07.01.1988 Bulletin 1988/01

(43) Date of publication A2:
21.10.1987 Bulletin 1987/43

(21) Application number: 87302097

(22) Date of filing: 11.03.1987
(84) Designated Contracting States:
AT BE CH DE ES FR GB IT LI NL SE

(30) Priority: 12.03.1986 GB 8606110
12.03.1986 GB 8606111
12.03.1986 GB 8606112
12.03.1986 GB 8606113
12.03.1986 GB 8606114
12.03.1986 GB 8606115

(71) Applicant: GLAXO GROUP LIMITED
 ()

(72) Inventors:
  • Rudd, Brian A. M.
     ()
  • Fletton, Richard A.
     ()
  • Ward, John B.
     ()
  • Noble, David
     ()
  • Porter, Neil
     ()
  • Lawrence, Gordon C.
     ()
  • Noble, Hazel M.
     ()

   


(54) Macrolide compounds


(57) Compounds of the formula

[wherein

R1 represents a methyl group;

R2 represents a methyl group

R3 represents a methyl, ethyl or isopropyl group; and

-A- represents a ring which is either

(where R4 is a hydroxy or methoxy group and R5 is a hydrogen atom or R4 and R5 together with the carbon atom to which they are attached represent a group C=0); or when -A-represents ring (ii) wherein R4 and R5 together with the carbon atom to which they are attached represent a group C=0 then R2 may also represent an aldehydo group;

or R2 represents a hydroxymethyl group and -A- represents

(where R6 represents a hydrogen atom or a hydroxy group);

(where R7 is a hydroxy or methoxy group and Z represents either a group CHOH or a group C=0);

or R1 represents a hydrogen atom and

(where R8 is a hydroxy or methoxy group); with the provisos that when R2 represents a methyl group and R4 represents a methoxy group then R3 cannot represents a methyl or isopropyl group and when R2 represents a hydroxymethyl group and R6 represents a hydroxy group then R3 cannot represent a methyl group.


Compounds of the invention have antiparasitic activity.





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